MX2013011947A - Iminotiazinas 5-sustituidas y sus monoxidos y dioxidos como inhibidores de la enzima que encinde la proteina precursora amiloide en el sitio beta, composiciones y su uso. - Google Patents

Iminotiazinas 5-sustituidas y sus monoxidos y dioxidos como inhibidores de la enzima que encinde la proteina precursora amiloide en el sitio beta, composiciones y su uso.

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Publication number
MX2013011947A
MX2013011947A MX2013011947A MX2013011947A MX2013011947A MX 2013011947 A MX2013011947 A MX 2013011947A MX 2013011947 A MX2013011947 A MX 2013011947A MX 2013011947 A MX2013011947 A MX 2013011947A MX 2013011947 A MX2013011947 A MX 2013011947A
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MX
Mexico
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alkyl
group
compound
mmol
tautomer
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MX2013011947A
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English (en)
Spanish (es)
Inventor
Jack D Scott
Duane A Burnett
Jared N Cumming
Eric J Gilbert
Andrew W Stamford
Wen-Lian Wu
Chad Edward Bennett
Younong Yu
Xuanjia Peng
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Merck Sharp & Dohme
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Publication of MX2013011947A publication Critical patent/MX2013011947A/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D279/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/101,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/121,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
MX2013011947A 2011-04-13 2012-04-12 Iminotiazinas 5-sustituidas y sus monoxidos y dioxidos como inhibidores de la enzima que encinde la proteina precursora amiloide en el sitio beta, composiciones y su uso. MX2013011947A (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201161475215P 2011-04-13 2011-04-13
US201161503254P 2011-06-30 2011-06-30
CN2012000435 2012-04-05
PCT/CN2012/000497 WO2012139425A1 (en) 2011-04-13 2012-04-12 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors,compositions,and their use

Publications (1)

Publication Number Publication Date
MX2013011947A true MX2013011947A (es) 2014-01-16

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013011947A MX2013011947A (es) 2011-04-13 2012-04-12 Iminotiazinas 5-sustituidas y sus monoxidos y dioxidos como inhibidores de la enzima que encinde la proteina precursora amiloide en el sitio beta, composiciones y su uso.

Country Status (9)

Country Link
US (1) US9499502B2 (cg-RX-API-DMAC7.html)
EP (1) EP2697210B1 (cg-RX-API-DMAC7.html)
JP (1) JP2014514302A (cg-RX-API-DMAC7.html)
AU (1) AU2012243329B2 (cg-RX-API-DMAC7.html)
BR (1) BR112013026341A2 (cg-RX-API-DMAC7.html)
CA (1) CA2832473A1 (cg-RX-API-DMAC7.html)
MX (1) MX2013011947A (cg-RX-API-DMAC7.html)
RU (1) RU2013150349A (cg-RX-API-DMAC7.html)
WO (1) WO2012139425A1 (cg-RX-API-DMAC7.html)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
EP2694521B1 (en) 2011-04-07 2015-11-25 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2694489B1 (en) 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
JP2014524472A (ja) * 2011-08-22 2014-09-22 メルク・シャープ・アンド・ドーム・コーポレーション Bace阻害剤としての2−スピロ置換イミノチアジンならびにそのモノオキシドおよびジオキシド、組成物、ならびにそれらの使用
NZ702254A (en) * 2012-05-24 2016-08-26 Hoffmann La Roche 5-amino[1,4]thiazines as bace 1 inhibitors
US9556135B2 (en) 2012-10-12 2017-01-31 Amgen, Inc. Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
WO2014093190A1 (en) 2012-12-14 2014-06-19 Merck Sharp & Dohme Corp. Bace inhibitors of iminothiadiazine dioxides
AU2013363151A1 (en) * 2012-12-20 2015-06-04 Merck Sharp & Dohme Corp. C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors
US9580396B2 (en) 2012-12-21 2017-02-28 Merck Sharp & Dohme Corp. C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use
WO2014120658A1 (en) 2013-01-29 2014-08-07 Amgen Inc. Fused multicyclic 3-amino-5,6-dihydro-2h-1,4-thiazine derivatives and their use as beta-secretase inhibitors
MX366855B (es) 2013-03-01 2019-07-26 Amgen Inc Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso.
CN105164121A (zh) 2013-03-08 2015-12-16 美国安进公司 作为β分泌酶抑制剂的全氟化环丙基稠合的1,3-噁嗪-2-胺化合物以及其使用方法
EP2968353B1 (en) * 2013-03-15 2018-12-19 Merck Sharp & Dohme Corp. C2-azaspiro iminothiazine dioxides as bace inhibitors
WO2014150340A1 (en) 2013-03-15 2014-09-25 Merck Sharp & Dohme Corp. S-imino-s-oxo iminothiadiazine compounds as bace inhibitors, compositions, and their use
EP2968357B1 (en) * 2013-03-15 2018-07-04 Merck Sharp & Dohme Corp. S-imino-s-oxo iminothiazine compounds as bace inhibitors, compositions, and their use
US9096615B2 (en) 2013-07-30 2015-08-04 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof
EP3083575B1 (en) * 2013-12-18 2021-11-03 Merck Sharp & Dohme Corp. C-6 spirocarbocyclic iminothiadiazine dioxides as bace inhibitors, compositions, and their use
EP3082823B1 (en) * 2013-12-18 2020-04-22 Merck Sharp & Dohme Corp. Iminothiadiazepane dioxide compounds as bace inhibitors, compositions, and their use
EP2918171A1 (en) * 2014-03-14 2015-09-16 University of Vienna Novel plant growth regulators and their use in modulating organ number
KR20180078347A (ko) 2014-04-10 2018-07-09 화이자 인코포레이티드 2-아미노-6-메틸-4,4a,5,6-테트라히드로피라노[3,4-d][1,3]티아진-8a(8H)-일-1,3-티아졸-4-일 아미드
US9732088B2 (en) 2014-06-02 2017-08-15 Merck Sharp & Dohme Corp. C2-carbocyclic iminothiazine dioxides as BACE inhibitors, compositions, and their use
US10047102B2 (en) 2014-07-25 2018-08-14 Hoffmann-La Roche Inc. Pyridyl-triazabicycles
EP3191447B1 (en) 2014-09-12 2019-05-01 Merck Sharp & Dohme Corp. S-imino-s-oxo iminothiazine compounds as bace inhibitors, compositions, and their use
EP3261442B1 (en) 2015-01-20 2020-04-01 Merck Sharp & Dohme Corp. Iminothiadiazine dioxides bearing an amine-linked substituent as bace inhibitors, compositions, and their use
MX2017012188A (es) 2015-03-20 2017-12-15 Hoffmann La Roche Inhibidores de beta-secretasa 1 (bace1).
JP6765681B2 (ja) * 2015-04-21 2020-10-07 オールジェネシス バイオセラピューティクス インコーポレイテッド Bace1阻害剤としての化合物およびそれらの使用
WO2017024180A1 (en) 2015-08-06 2017-02-09 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
WO2017051303A1 (en) 2015-09-24 2017-03-30 Pfizer Inc. Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors
EP3353183A1 (en) 2015-09-24 2018-08-01 Pfizer Inc N-[2-(2-amino-6,6-disubstituted-4, 4a, 5, 6-tetrahydropyrano [3,4-d][1,3]thiazin-8a (8h)-yl) -1, 3-thiazol-4-yl]amides
TW201718581A (zh) 2015-10-19 2017-06-01 英塞特公司 作為免疫調節劑之雜環化合物
CA3005727A1 (en) 2015-11-19 2017-05-26 Incyte Corporation Substituted 2-methylbiphenyl-3-yl heterocyclic compounds and pharmaceutical compositions thereof useful as immunomodulators
WO2017095759A1 (en) 2015-12-04 2017-06-08 Merck Sharp & Dohme Corp. C5-c6-carbocyclic fused iminothiadiazine dioxides as bace inhibitors, compositions, and their use
TW201726623A (zh) * 2015-12-17 2017-08-01 英塞特公司 作為免疫調節劑之雜環化合物
CR20180374A (es) 2015-12-22 2018-10-16 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
MA44860A (fr) 2016-05-06 2019-03-13 Incyte Holdings Corp Composés hétérocycliques utilisés comme immunomodulateurs
US20170342060A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
CA3028685A1 (en) 2016-06-20 2017-12-28 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018013789A1 (en) 2016-07-14 2018-01-18 Incyte Corporation Heterocyclic compounds as immunomodulators
ES2941716T3 (es) 2016-08-29 2023-05-25 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
US11021493B2 (en) 2016-12-15 2021-06-01 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
AU2017376441B2 (en) 2016-12-15 2021-10-14 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
JP7148518B2 (ja) 2016-12-15 2022-10-05 アムジエン・インコーポレーテツド β-セクレターゼ阻害剤としての二環式チアジンおよびオキサジン誘導体ならびに使用方法
AU2017378316B2 (en) 2016-12-15 2021-04-01 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
CA3047288A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
JP7303108B2 (ja) 2016-12-22 2023-07-04 インサイト・コーポレイション 免疫調節剤としての二環式複素芳香環化合物
CR20190318A (es) 2016-12-22 2019-10-21 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
SG10202106743QA (en) 2016-12-22 2021-08-30 Incyte Corp Tetrahydro imidazo[4,5-c]pyridine derivatives as pd-l1 internalization inducers
US20180179201A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
ES2899402T3 (es) 2016-12-22 2022-03-11 Incyte Corp Derivados de piridina como inmunomoduladores
KR102717600B1 (ko) 2017-10-06 2024-10-15 포르마 세라퓨틱스 인크. 유비퀴틴 특이적 펩티다제 30의 억제
CN111511732A (zh) * 2017-12-21 2020-08-07 豪夫迈·罗氏有限公司 放射性标记化合物
JP7590183B2 (ja) 2018-03-13 2024-11-26 武田薬品工業株式会社 血漿カリクレインのインヒビターとしての置換されたイミダゾピリジン及びその使用
EP4212529B1 (en) 2018-03-30 2025-01-29 Incyte Corporation Heterocyclic compounds as immunomodulators
BR112020021728A2 (pt) 2018-04-27 2021-01-26 Shionogi & Co., Ltd. derivados de tetra-hidropiranooxazina tendo atividade inibitória de bace1 seletiva
EP4520328A3 (en) 2018-05-11 2025-04-16 Incyte Corporation Heterocyclic compounds as immunomodulators
CA3098628A1 (en) 2018-05-17 2019-11-21 Forma Therapeutics, Inc. Fused bicyclic compounds useful as ubiquitin-specific peptidase 30 inhibitors
CN108997328B (zh) * 2018-09-06 2021-06-08 广东东阳光药业有限公司 亚氨基噻二嗪二氧化物衍生物及其用途
PT3860989T (pt) 2018-10-05 2023-06-30 Forma Therapeutics Inc Pirrolinas fundidas que atuam como inibidores da protease 30 específica da ubiquitina (usp30)
WO2021030162A1 (en) 2019-08-09 2021-02-18 Incyte Corporation Salts of a pd-1/pd-l1 inhibitor
CN114258392A (zh) * 2019-08-21 2022-03-29 卡尔维斯塔制药有限公司 酶抑制剂
WO2021055589A1 (en) 2019-09-18 2021-03-25 Shire Human Genetic Therapies, Inc. Heteroaryl plasma kallikrein inhibitors
WO2021055621A1 (en) 2019-09-18 2021-03-25 Shire Human Genetic Therapies, Inc. Plasma kallikrein inhibitors and uses thereof
CR20220190A (es) 2019-09-30 2022-06-15 Incyte Corp Compuestos de pirido [3,2-d] primidina como inmunomoduladores
EP4058461A1 (en) 2019-11-11 2022-09-21 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
PE20231438A1 (es) 2020-11-06 2023-09-14 Incyte Corp Proceso para hacer un inhibidor de pd-1/pd-l1 y sales y formas cristalinas del mismo
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
CA3256688A1 (en) 2022-04-28 2025-04-22 Kyoto Pharmaceutical Industries, Ltd. BENZOTRIAZOLE COMPOUND

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5534520A (en) 1990-04-10 1996-07-09 Fisher; Abraham Spiro compounds containing five-membered rings
US7488756B2 (en) * 2001-01-23 2009-02-10 Neurosearch A/S Use of non-competitive and selective GluR5 antagonists as glutamate receptor modulating compounds
WO2004094382A1 (en) 2003-03-21 2004-11-04 Eli Lilly And Company Muscarinic agonists
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) * 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US8436006B2 (en) * 2004-08-06 2013-05-07 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
WO2006041404A1 (en) * 2004-10-15 2006-04-20 Astrazeneca Ab Substituted amino-compounds and uses thereof
JP5281794B2 (ja) 2005-10-25 2013-09-04 塩野義製薬株式会社 アミノジヒドロチアジン誘導体
TW200808751A (en) 2006-04-13 2008-02-16 Astrazeneca Ab New compounds
JP2009539983A (ja) 2006-06-12 2009-11-19 シェーリング コーポレイション 複素環式アスパルチルプロテアーゼ阻害薬
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
EP2147914B1 (en) 2007-04-24 2014-06-04 Shionogi&Co., Ltd. Aminodihydrothiazine derivatives substituted with cyclic groups
US20110009392A1 (en) 2007-08-06 2011-01-13 Schering Corporation Gamma secretase modulators
TW201004957A (en) 2008-04-22 2010-02-01 Schering Corp Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as bace-1 inhibitors, compositions, and their use
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Bace抑制劑
JP5490692B2 (ja) 2008-06-13 2014-05-14 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
AR077328A1 (es) 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
US20110065695A1 (en) 2009-09-11 2011-03-17 Jeremy Beauchamp Use of aminodihydrothiazines for the treatment or prevention of diabetes
EP2485590B1 (en) 2009-10-08 2015-01-07 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
UA108363C2 (uk) * 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
JPWO2011058763A1 (ja) 2009-11-13 2013-03-28 塩野義製薬株式会社 アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体
US20120245154A1 (en) 2009-12-09 2012-09-27 Shionogi & Co., Ltd. Substituted aminothiazine derivative
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
UA103272C2 (uk) 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2
WO2011077726A1 (ja) 2009-12-24 2011-06-30 塩野義製薬株式会社 4-アミノ-1,3-チアジンまたはオキサジン誘導体
SG181431A1 (en) 2009-12-31 2012-07-30 Novartis Ag Pyrazine derivatives and their use in the treatment of neurological disorders
US8673894B2 (en) 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds
AR081389A1 (es) 2010-05-12 2012-08-29 Astrazeneca Ab Sal de tipo hemifumarato, composicion farmaceutica y proceso de obtencion de la misma.
JP5711813B2 (ja) 2010-06-09 2015-05-07 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap βセクレターゼ(BACE)の阻害剤として有用な5,6−ジヒドロ−2H−[1,4]オキサジン−3−イル−アミン誘導体
EA201291366A1 (ru) 2010-06-09 2013-04-30 Янссен Фармацевтика Нв Производные 5-амино-3,6-дигидро-1h-пиразин-2-она в качестве ингибиторов бета-секретазы (bace)
RS53096B (sr) 2010-07-13 2014-06-30 Novartis Ag Derivati oksazina i njihova upotreba u lečenju neuroloških oboljenja
US8815881B2 (en) 2010-08-09 2014-08-26 Hoffmann-La Roche Inc. 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders

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BR112013026341A2 (pt) 2019-09-24

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